Skip Header

You are using a version of browser that may not display all the features of this website. Please consider upgrading your browser.

Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.

Anderson K., Chen Y., Chen Z., Dominique R., Glenn K., He Y., Janson C., Luk K.C., Lukacs C., Polonskaia A., Qiao Q., Railkar A., Rossman P., Sun H., Xiang Q., Vilenchik M., Wovkulich P., Zhang X.

DYRK1B is a kinase over-expressed in certain cancer cells (including colon, ovarian, pancreatic, etc.). Recent publications have demonstrated inhibition of DYRK1B could be an attractive target for cancer therapy. From a data-mining effort, the team has discovered analogues of pyrido[2,3-d]pyrimidines as potent enantio-selective inhibitors of DYRK1B. Cells treated with a tool compound from this series showed the same cellular effects as down regulation of DYRK1B with siRNA. Such effects are consistent with the proposed mechanism of action. Progress of the SAR study is presented.

Bioorg. Med. Chem. Lett. 23:6610-6615(2013) [PubMed] [Europe PMC]

We'd like to inform you that we have updated our Privacy Notice to comply with Europe’s new General Data Protection Regulation (GDPR) that applies since 25 May 2018.

Do not show this banner again
UniProt is an ELIXIR core data resource
Main funding by: National Institutes of Health